Antimycobacterials Flashcards

1
Q

What is the MOA of Isoniazid?

A

Inhibits biosynthesis of mycolic acid (component of cell wall)

Requires KatG for activation

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2
Q

What are the uses of Isoniazid?

A

Mycobacterium tuberculosis (both active and latent)

Must be used with RIF, EMB, and PZA in active TB

Can be used alone in latent TB

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3
Q

What are toxicities of Isoniazid?

A
  • Hepatotoxicity (fast acetylators)
  • Peripheral neuritis (slow acetylators)
  • Hemolysis (G6PD deficiency)
  • Lupus like syndrome (HIP drug)
  • Seizures, insomnia
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4
Q

What is the DOC for Mycobacterium tuberculosis?

A

Isoniazid

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5
Q

What is the MOA for Rifampin?

A

Inhibits DNA dependent RNA polymerase

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6
Q

What are the uses of Rifampin?

A
  • Mycobacterium tuberculosis (both active and latent)
  • Mycobacterium avium complex (MAC)
  • Mycobacterium leprae

(Must be used with INH, EMB, and PZA in active TB)

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7
Q

What are toxicities of Rifampin?

A
  • Hepatic enzyme induction (cytochrome P450s)
  • Decreased effectiveness of birth control
  • Orange color to secretions
  • GI disturbances
  • Hypersensitivity/allergy
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8
Q

What population should Rifampin be avoided in?

A

HIV-treated individuals

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9
Q

What is the DOC for Mycobacterium leprae?

A

Rifampin + Dapsone

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10
Q

What is the MOA for Ethambutol?

A

Inhibits arabinosyl transferase involved in the synthesis of arabinogalactan (in cell wall)

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11
Q

What are the uses of Ethambutol?

A
  • Mycobacterium tuberculosis (TB)

- Mycobacterium avium complex (MAC)

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12
Q

What combination of drugs can be used to treat Mycobacterium avium complex (MAC)?

A

Ethambutol + clarithromycin + rifabutin/rifampin/cipro

OR

Ethambutol + azithromycin + rifabutin/rifampin/cipro

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13
Q

What are major toxicities of Ethambutol

A
  • Decreased visual acuity and loss of green-red perception

- Renal insufficiency (give smaller dose)

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14
Q

What population should Ethambutol be avoided in?

A

Children under 13 years of age due to adverse effects on vision

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15
Q

When is Pyrazinamide active and when does it have its greatest activity?

A

Active in acidic pH

Has greatest activity against dormant organisms

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16
Q

What are the uses of Pyrazinamide?

A

Mycobacterium tuberculosis (optimal within macrophages due to activity at acidic pH)

(Must be given with INH, RIF, and EMB in active TB)

17
Q

What are toxicities of Pyrazinamide?

A
  • Hepatic dysfunction
  • Hyperuricemia (lead to gout flares)
  • GI, myalgia, photosensitivity, porphyria
18
Q

What is the MOA of Rifabutin?

A

Inhibits DNA dependent RNA polymerase

19
Q

What are the uses of Rifabutin?

A
  • Active Mycobacterium tuberculosis with co-infection of HIV
  • Mycobacterium avium complex (MAC)
20
Q

What is the DOC for Mycobacterium tuberculosis WITH co-infection of HIV?

A

Rifabutin

21
Q

What is an advantage of Rifabutin over Rifampin?

A

Rifabutin is a less potent inducer of P450 enzymes

22
Q

What is the MOA of Rifapentine?

A

Inhibits DNA dependent RNA polymerase

23
Q

What are the uses of Rifapentine?

A

Latent Mycobacertium tuberculosis (including HIV+ patients)

24
Q

What is the DOC for LATENT Mycobacertium tuberculosis (including HIV+)?

A

Isoniazid + Rifapentine

25
Q

What is the MOA for Dapsone?

A

PABA antagonist

26
Q

What are the uses of Dapsone?

A

Mycobacterium leprae (+ RIF)

27
Q

What are the toxicities of Dapsone?

A
  • Nasal obstruction (improves in 3-6 months)
  • Dose related hemolysis
  • Agranulocytosis
  • Peripheral neuritis
28
Q

What are the uses of Thalidomide?

A

Moderate to severe ENL

29
Q

What are toxicities of Thalidomide?

A

Teratogenic!

30
Q

What is the DOC for moderate to severe ENL?

A

Thalidomide

31
Q

What drugs are used for Latent TB?

A
  • INH monotherapy
  • Rifampin monotherapy
  • Rifapentine + INH